Digitoxin has specific properties for potential use to treat cancer and inflammatory diseases

Haux, Johan

doi:10.32474/rrhoaj.2018.02.000137

Cited by 3 publications

(1 citation statement)

References 21 publications

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“…Novel complementary treatments are warranted since current treatments are often inefficient and are associated with severe side-effects (3). Data from epidemiological studies have suggested positive therapeutic effects using cardiac glycosides in the treatment of various types of cancer, and may thus prove to be promising as a complementary treatment to current PDAC therapeutics (4)(5)(6)(7).…”

Section: Introductionmentioning

confidence: 99%

Na+/K+‑ATPase subunit α3 expression is associated with the efficacy of digitoxin treatment in pancreatic cancer cells

Lindholm

Ejeskär

Szekeres

2022

Med Int

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the alpha subunits (atP1a1-3) of Na + /K + -atPase binds digitoxin with varying affinity. The expression levels of these subunits dictate the anticancer effects of digitoxin. In the present study, three pancreatic cancer cell lines, asPC-1, Panc-1 and CFPaC-1, were used to investigate the effects of digitoxin in relation to the expression of the subunits ATP1A1 and ATP1A3. Cell viability and intracellular calcium concentrations was measured in relation to the gene and protein expression of ATP1A1 and ATP1A3. Digitoxin was used to treat the cells at concentrations of 1-100 nM, and the intracellular calcium concentrations increased in a concentration-dependent manner in the Panc-1 and in the CFPAC-1 cells with treatment at 100 nM. In the AsPC-1 cells only the supraphysiological concentration of digitoxin (100 nM) resulted in a decrease in the number of viable cells (unviable cells increased to 22%), whereas it had no effect on intracellular calcium levels. The number of viable Panc-1 and CFPaC-1 cells decreased after digitoxin treatment at 25-100 nM (unviable Panc-1 cells increased to 33-59%; unviable CFPAC-1 cells increased to 22-56%). Digitoxin treatment also affected the transcriptional expression of the ATP1A1 and ATP1A3 subunits. In Panc-1 cells, ATP1A3 gene expression was negatively associated with the digitoxin concentration (25-100 nM). In the AsPC-1 and CFPAC-1 cells, the expression of the ATP1A1 gene increased in the cells treated with the 100 nM digitoxin concentration. The protein expression of atP1a1 and atP1a3 was not altered with digitoxin treatment. The basal protein expression of ATP1A1 was high in the asPC-1 and CFPaC-1 cells, compared to the Panc-1 cells, in contrast to the basal expression of atP1a3, which was higher in the Panc-1 cells, compared to the other pancreatic cancer cells used. On the whole, the present study demonstrates that the high expression of atP1a3 renders pancreatic cancer cells more susceptible to digitoxin-induced cell death. The findings suggest that the expression of ATP1A3 may be used as a marker for tumor sensitivity to digitoxin treatment, where a high expression of atP1a3 is favorable for the anticancer effects of digitoxin.

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Section: Introductionmentioning

confidence: 99%

Na+/K+‑ATPase subunit α3 expression is associated with the efficacy of digitoxin treatment in pancreatic cancer cells

Lindholm

Ejeskär

Szekeres

2022

Med Int

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Virtual Screening of Inhibitors Against Spike Glycoprotein of SARS-CoV-2: A Drug Repurposing Approach

Senathilake¹,

Samarakoon²,

Tennekoon³

2020

Preprint

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The novel coronavirus (SARS-CoV-2) is a human pathogen recently emerged in China, causing a global pandemic of severe respiratory illness (COVID19). SARS-CoV-2 makes entry into human cells through its spike (S) protein that binds to cell surface receptors. Widespread of SARS-CoV-2 has been attributed to high affinity of S protein to its receptor. A homology model of the receptor binding domain of SARS-CoV-2 S protein (RBD) was built. RBD- receptor docking and published molecular dynamics data were used to map the key RBD-receptor interaction hotspot (RBDhp) on the RBD. Primary virtual screening was carried out against RBDhp using more than 3300 compounds approved by U.S Food and Drug Administration (FDA) and other authorities for human use. Compounds that bind to hpRBD with a binding energy ≤ - 6.5 kcal/mol were subjected to secondary screening using a recently published cryo EM (2.9 Å) structure of RBD. A cardiac glycoside (dgitoxin), two anthracyclines (zorubicin and aclarubicin), a tetracycline derivative (rolitetracycline), a cephalosporin (cefoperazone) and a food dye (E-155) were predicted to be most potent inhibitors of RBD – receptor interaction. An anti-asthmatic drug (zafirlukast) and several other drugs (itrazol, fazadinium, troglitazone, gliquidone, Idarubicin, Oxacillin) were found to be high affinity binders that may have a potential to inhibit RBD – receptor interaction.

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Transformation in Content of Bioactive Compounds of Glodok Fish (Boleopthalmus boddarti) Based on the Effect of Variations in Temperature and Frying Time

Ridho¹,

Patriono²,

Cahyani³

et al. 2023

CBC

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Objective: One species of glodok fish is Boleophthalmus boddarti. The fish was identified to contain bioactive compounds such as steroids, terpenoids, bufadienolid, carotatoksin, and corticosteroids. Bioactive compounds have benefits for human life. Methods: Lampung coastal communities consume glodok fish to cure asthma. They consume glodok fish by various processing methods, such as by frying. The frying process is expected to damage some nutrients such as vitamins and proteins, including the possibility of damaging bioactive compounds. However, there is no data regarding the effect of using different temperatures and times in the frying process on changes in bioactive content in the meat of the glodok fish. Sampling was carried out around the mouth of the Musi River, South Sumatra. The stages of the research consisted of the preparation process, treatment using 9 variations of temperature and frying time, sample extraction, analysis of the content of bioactive compounds by GC-MS. Results: The results showed that the bioactive compounds identified before fried fishes consisted of corticosteroids, steroids, carotenoids, monoterpenoids, sesquiterpenoids, and triterpenoids. Conclusion: Variations in the treatment resulted in cholesterol of the steroid group in the highest treatment at 14.36% and the loss of betamethasone acetate compounds in the corticosteroid group by 0.07% in the treatment sample.

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Digitoxin has specific properties for potential use to treat cancer and inflammatory diseases

Cited by 3 publications

References 21 publications

Na+/K+‑ATPase subunit α3 expression is associated with the efficacy of digitoxin treatment in pancreatic cancer cells

Na+/K+‑ATPase subunit α3 expression is associated with the efficacy of digitoxin treatment in pancreatic cancer cells

Virtual Screening of Inhibitors Against Spike Glycoprotein of SARS-CoV-2: A Drug Repurposing Approach

Transformation in Content of Bioactive Compounds of Glodok Fish (Boleopthalmus boddarti) Based on the Effect of Variations in Temperature and Frying Time

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